viii New Patents

4994456 4994471

P Y R I D I N E C A R B O X Y L I C A C I D A M I D E D E R I V A T I V E S A N D

P H A R M A C E U T I C A L C O M P O S I T I O N S C O M P R I S I N G

S A M E

Katsutosh Miura, Hiroyasu Koyama, Toshiji Sugai, Hiroaki Yamada, Einosuk Sakurai, Masato Horigome, Saitama, Japan assigned to Nisshin Flour Milling Co Ltd

Compounds are disclosed of the formula See Pa- tent for Chemical Structure (I) wherein R1 is hydrogen; C1-C6 alkyl; C3-C6 cycloalkyl or diphenylmethyl; Y is -NH(CH2)n-R2 or See Pa- tent for Chemical Structure R2 is OH or -ONO2; 1 is 2 or 3; m is 0 or 1; and n is 2 to 8; and phys- iologically acceptable acid addition salts thereof. The compounds of formula (I) are of a blood flow-increasing and hypotensive actions and can be used for the therapy or prevention of diseases in the cardiovascular system.

4994470

B E N Z O P Y R A N D E R I V A T I V E S A N D P H A R M A C E U T I C A L

C O M P O S I T I O N S C O N T A I N I N G T H E M

Michel Barreau, Jean-Claude Hardy, Christian Renault, Montgeron, France assigned to Rhone- Poulenc Sante

New benzopyran derivatives of general formula (I) in which: R1 denotes a hydrogen or halogen atom or a hydroxy, alkyloxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, or acylamino radical, R denotes a radical of general formula: See Patent for Chemical Struc- ture in which A denotes a single bond or a methy- lene radical and R2 and R3 which may be identical or different, denote a hydrogen or halogen atom or a hydroxy, alkyl, alkyloxy, nitro, amino, alkylsulphonamido, bi- s(alkylsulphonyl)amino, acylamino, sulphamoyl or cyano radical, or form together, when they are adjacent, a methylenedioxy or ethylenedioxy radical, or alternatively R denotes a 2-oxo-2H- benzimidazolyl radical, and R' and R" are iden- tical and denote hydrogen atoms or alkyl radicals, their isomeric forms and their prepara- tion. These new products are useful as anti- arrhythmic and antifibrillating agents. See Patent for Chemical Structure (I)

N - A R Y L - N - ( 1 S U B S T I T U T E D - 3 A L K O X Y - 4 P I P E R I D I N Y L ) A M I D E S

A N D P H A R M A C E U T I C A L C O M P O S I T I O N S A N D M E T H O D S

E M P L O Y I N G S U C H C O M P O U N D S

Nhora L Lalinde, Joh Moliterni, H Kenneth Spencer assigned to BOC Inc

This invention pertains to novel N-aryl-N-(N- substituted 3-alkoxy-4-piperidinyl)amides use- ful as analgesics, and methods of administering analgesia, which comprises the systemic ad- ministration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: See Patent for Chem- ical Structure (I) including optically active isomeric forms, cis/trans isomeric forms and the pharmaceutically acceptable acid addition salts therof, wherein: R is an aryl group selected from the group consisting of phenyl and substituted phenyl, wherein the substituents on the phenyl group are independently selected from the group consisting of halogen, lower-alkyl, lower- alkoxy, and combinations thereof; R1 is an alkyl group selected from the group consisting of lower-alkyl, lower-alkenyl, and lower-alkoxy lower-alkyl, each alkyl group having from 1 to 6 carbon atoms; R2 is a member selected from the group consisting of phenyl lower-alkyl, thienyl lower-alkyl, pyrazolyl lower-alkyl, tetrazolyl lower-alkyl, 4, 5-dihydro-5-oxo-lH-tetrazolyl lower-alkyl, 1,3-dihydro-l, 3-dioxo-2H- isoindolyl lower-alkyl, and 2, 3-dihydro-2-oxol H-benzimidazolyl lower-alkyl; and R3 is a mem- ber selected from the group consisting of hydro- gen, lower-alkyl and lower-alkyl aryl.

4994493

N - S U B S T I T U T E D 5- N I T R O A N T H R A N I L I C A C I D S , A

P R O C E S S F O R T H E I R P R E P A R A T I O N , T H E I R U S E , A N D P H A R M A C E U T I C A L P R O D U C T S B A S E D O N T H E S E C O M P O U N D S

Raine Greger, Heinrich C Englert, Hans-Jochen Lang, Max Hropot, Heitersheim, Federal Republic Of Germany assigned to Max-Planck- Gesellschaft zur Forderung der Wissenschaften; Hoechst Aktiengesellscha